环孢素A固体脂质纳米粒制备工艺优化

Optimization of the preparation of cyclosporine SLN

为了制备单分散性优良、形态规整且具有较高包封率的环孢素A固体脂质纳米粒,采用溶剂扩散法制备环孢素A固体脂质纳米粒。在水相中加入海藻酸钠以改善纳米粒形态和单分散性,利用Ca2+与载药纳米粒胶体溶液中海藻酸钠发生配位反应形成海藻酸钙凝胶,在低离心转速下分离纳米粒并简便准确测定药物包封率。在单因素实验基础上,采用响应面设计优化载药纳米粒的制备工艺条件。结果表明,影响包封率显著因素为水含量和制备温度,在海藻酸钠用量0.1132 g、用水量52.77 mL、制备温度34.55℃优化条件下,纳米粒形态呈规整棒状,单分散性好,平均粒径为181.3 nm,平均包封率达82.45%。

To investigate the preparation of cyclosporine A-loaded SLN with good monodispersity,regular shape and higher entrapment efficiency.Cyclosporine A-loaded SLN was prepared by solvent diffusion method.The shape and monodispersity of Cyclosporine A-loaded SLN was improved by adding some sodium alginate in the aqueous phase.Due to the formation of calcium alginate gel by adding Ca2＋ into solution containing sodium alginate,cyclosporine A-loaded SLN could be separated at low speed of centrifugation and the entrapment efficiency could be determined easily and exactly.Based on single factor experiments,optimal conditions were gained by response surface design.Water content and aqueous temperature were significant factors for encapsulation efficiency.With the optimal condition,i.e.0.1132 g sodium alginate,52.77mL water content and 34.55 ℃ aqueous temperature,cyclosporine A-loaded SLN was prepared with rod-like shape and satisfied monodisperse.The average size was 181.3nm and the average entrapment efficiency was 82.45%.